Miyazaki Yasushi, Maeda Yutaka, Sato Hideyuki, Nakano Masato, Mellor Geoffrey W
GlaxoSmithKline, Tsukuba Research Laboratories, Chemistry Department, 43, Wadai, Tsukuba, Ibaraki 300-4247, Japan.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1967-71. doi: 10.1016/j.bmcl.2008.01.113. Epub 2008 Feb 2.
4-Amino-5,6-diaryl-furo[2,3-d]pyrimidines have been identified as inhibitors of glycogen synthase kinase-3beta (GSK-3beta). One representative derivative, 4-amino-3-(4-(benzenesulfonylamino)-phenyl)-2-(3-pyridyl)-furo[2,3-d]pyrimidine (12) exhibited potent GSK-3beta inhibitory activity in low nanomolar level of IC(50). The binding mode was proposed from a docking study.
4-氨基-5,6-二芳基呋喃并[2,3-d]嘧啶已被鉴定为糖原合酶激酶-3β（GSK-3β）的抑制剂。一种代表性衍生物，4-氨基-3-(4-(苯磺酰氨基)-苯基)-2-(3-吡啶基)-呋喃并[2,3-d]嘧啶（12）在低纳摩尔水平的IC50下表现出强效的GSK-3β抑制活性。通过对接研究提出了其结合模式。
